Enteric coating for targeting the duodenum

Abstract

A system for targeted delivery of a medicament to the gastrointestinal tract (e.g., selectively to the duodenum) of a subject. The system includes a medicament, a mucoadhesive layer at least partially surrounding the medicament, and an enteric coating encasing the medicament and mucoadhesive layer. The enteric coating comprises a material degradable by a pH of the GI tract and a material digestible by a lipase. Also provided are method of making and using the system for targeted delivery of a medicament to the gastrointestinal tract. Also provided are a system for deploying a medicament-containing needle system using an expanding element. The system includes a medicament-containing needle system and an expanding element within a capsule. The capsule is initially coated with an enteric coating. As the enteric coating degrades the expanding element absorbs fluid that enters the capsule and expands to deploy the medicament-containing needle system from the capsule.

1 . A method of making a system for targeted delivery of a medicament to a gastrointestinal (GI) tract of a subject, comprising:
 (a) providing a medicament;   (b) at least partially coating the medicament with a mucoadhesive layer to provide a mucoadhesive-coated medicament;   (c) at least partially coating the mucoadhesive-coated medicament with a material degradable by a pH of the GI tract; and   (d) at least partially coating the mucoadhesive-coated medicament with a material digestible by a lipase.   
     
     
         2 . The method of  claim 1 , wherein steps (c) and (d) are performed concurrently. 
     
     
         3 . The method of  claim 2 , wherein steps (c) and (d) comprises coating the mucoadhesive-coated medicament with a composition comprising the material degradable by a pH of the GI tract and the material digestible by a lipase in a ratio of 1:1, 0.6:0.4, 0.4:0.6, 0.7:0.3, 0.3:0.7. 
     
     
         4 . The method of  claim 1 , wherein steps (c) and (d) are performed separately. 
     
     
         5 . The method of  claim 4 , wherein steps (c) and (d) result in a 1:1, 0.6:0.4, 0.4:0.6, 0.7:0.3, 0.3:0.7 ratio of the material degradable by a pH of the GI tract and the material digestible by a lipase coating the mucoadhesive-coated medicament. 
     
     
         6 . The method of  claim 2 , wherein the material degradable by a pH of the GI tract comprises a polymer. 
     
     
         7 . The method of  claim 2 , wherein the material digestible by a lipase comprises a wax material. 
     
     
         8 . The method of  claim 2 , further comprising providing an expanding material and wherein providing the medicament comprises providing a needle delivery system, the expanding material expandable to deploy the needle delivery system out of the mucoadhesive layer. 
     
     
         9 . A method of administering a medicament directly to the gastrointestinal (GI) tract of a subject, administering to the subject a system for targeted delivery of a medicament to a gastrointestinal (GI) tract of a subject, comprising:
 (a) a medicament;   (b) a mucoadhesive layer at least partially surrounding the medicament; and   (c) an enteric coating encasing the medicament and mucoadhesive layer, wherein the enteric coating comprises a material degradable by a pH of the GI tract and a material digestible by a lipase.   
     
     
         10 . The method of  claim 9 , wherein the system is administered orally to the subject. 
     
     
         11 . The method of  claim 9 , wherein the medicament is administered selectively to the GI tract of the subject. 
     
     
         12 . The method of  claim 11 , wherein the medicament is administered selectively to the duodenum of the subject. 
     
     
         13 . A method of making a system for targeted delivery of a medicament to a gastrointestinal (GI) tract of a subject, comprising:
 (a) providing a medicament;   (b) providing an expanding material; and   (c) at least partially enclosing the medicament and the expanding material with a capsule.   
     
     
         14 . The method of  claim 13 , wherein:
 (a) the medicament comprises an array of microneedles and a mechanical actuator;   (b) the mechanical actuator, upon release from constraint by the capsule, expands outwardly in a direction away from a central longitudinal axis of the mechanical actuator and drives the array of microneedles into penetrating engagement with a lining of the GI tract of the subject;   (c) and wherein the penetrating engagement facilitates delivery of a payload via the microneedles.   
     
     
         15 . The method of  claim 13 , wherein providing the expanding material comprises providing an expanding material and a piston, the expanding material and the medicament on opposing sides of the piston. 
     
     
         16 . The method of  claim 13 , wherein the expanding material is a bio-compatible super absorbent material. 
     
     
         17 . The method of  claim 13 , wherein enclosing the medicament and the expanding material with the capsule comprises introduction into a pre-made capsule or application of coatings to form the capsule. 
     
     
         18 . The method of  claim 13 , wherein the capsule comprises a mucoadhesive layer or an enteric coating. 
     
     
         19 . The method of  claim 13 , wherein the capsule comprises a mucoadhesive layer and an enteric coating.